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Iranian Journal of Nuclear Medicine، جلد ۲۳، شماره ۱، صفحات ۳۶-۴۳
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عنوان انگلیسی Preparation and preliminary biological evaluation of [153Sm] samarium AMD3100; towards a possible therapeutic chemokine receptor CXCR4 targeting complex
چکیده انگلیسی مقاله Introduction: In continuation of recent development of possible C-X-C chemokine receptor type 4 (CXCR4) imaging agents, we report the development of a possible CXCR4 targeted therapy agent. Methods: [153Sm]labeled 1,1′-[1,4-phenylenebis(methylene)] bis-1,4,8,11-tetraazacyclo -tetradecane ([153Sm]-AMD3100) was prepared using [153Sm]SmCl3 and AMD-3100 for 24h at 50°C in acetate buffer.Stability tests, partition coefficient determination, toxicity tests and biodistribution studies of the complex in wild-type rats were determined. Results: The radiolabeled complex was prepared in high radiochemical purity (>95%; RTLC and >99% HPLC) and specific activity of 278 GBq/mmol and demonstrated significant stability up to 48h at 37 °C (in presence of human serum). Partition coefficient determination was calculated Log P= -1.09.Hepatotoxicity experiments demonstrated no distinguishable effect on hepatic enzymes in 10 days post injection.Initial complex biodistribution data showed significant liver and kidney accumulation in wild-type rats. Conclusion: Since lung and spleen are considered as CXCR4 rich organs, the best lung/blood and spleen/blood ratios were achieved 12 and 7 at 24 h post injection. Further investigations are needed especially on therapeutic properties of this agent.
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نویسندگان مقاله ایوب آقانژاد |
research center for nuclear medicine, tehran university of medical sciences, tehran, iran and department of nuclear pharmacy, faculty of pharmacy, tehran university of medical sciences, tehran, iran
سازمان اصلی تایید شده: دانشگاه علوم پزشکی تهران (Tehran university of medical sciences)

امیررضا جلیلیان | amir reza
nuclear science research school, nuclear science and technology research institute, tehran, iran

علی بهرامی سامانی | bahrami samani
nuclear science research school, nuclear science and technology research institute, tehran, iran

داود بیکی |
research center for nuclear medicine, tehran university of medical sciences, tehran, iran and department of nuclear pharmacy, faculty of pharmacy, tehran university of medical sciences, tehran, iran
سازمان اصلی تایید شده: دانشگاه علوم پزشکی تهران (Tehran university of medical sciences)

استپان maus |
clinic of nuclear medicine, university medical centre mainz, langenbeckstrasse 1, d-55131 mainz, germany

علی خلج |
department of nuclear pharmacy, faculty of pharmacy, tehran university of medical sciences, tehran, iran
سازمان اصلی تایید شده: دانشگاه علوم پزشکی تهران (Tehran university of medical sciences)

نشانی اینترنتی http://irjnm.tums.ac.ir/article_10764_614cd7007b1a06f6156f752ca1d014ab.pdf
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